Regioselective ruthenium-catalyzed carbonylative direct arylation of five-membered and condensed heterocycles.

A ruthenium-catalyzed carbonylative CH bond arylation process for the three-component synthesis of complex aryl-(hetero)aryl ketones in an aqueous solution has been developed. By exploiting the ortho-activating effect of nitrogen-containing directing groups, a regioselective, successive twofold C(sp(2))-C(sp(2)) bond formation has been achieved. This straightforward catalytic process provides access to versatile products prevalent in multiple bioactive compounds and supplies a valuable functional group for subsequent transformations.